Target intelligence / Profile preview

Adiponectin receptor 1 or Adiponectin receptor 2 (AdipoR1, AdipoR2)

Target
AdipoR1, AdipoR2
Molecular classification
Receptor, Seven-transmembrane receptor (distinct from classical GPCRs), PAQR (Progesterone/Adiponectin Q receptor) family
01

Overview

Adiponectin receptors 1 and 2 (AdipoR1 and AdipoR2) are seven-transmembrane proteins belonging to the PAQR family that mediate the metabolic and anti-inflammatory effects of adiponectin, an adipokine secreted by adipose tissue. AdipoR1 is highly expressed in skeletal muscle, while AdipoR2 predominates in the liver. Upon binding adiponectin, these receptors activate signaling cascades such as the AMPK and PPAR-α pathways, leading to increased fatty acid oxidation, reduced hepatic gluconeogenesis, improved insulin sensitivity, and anti-inflammatory actions. Their dysfunction is implicated in obesity, type 2 diabetes, and cardiovascular disease. No drugs are yet clinically approved to target these receptors, but AdipoRon, an experimental agonist, mimics some adiponectin effects. "Adiponectin receptor pathway" refers to this network of biochemical signals initiated by adiponectin binding to its receptors, rather than a single molecular entity.

Other names
AdipoR1AdipoR2Adiponectin receptorPAQR1 (AdipoR1)PAQR2 (AdipoR2)Progesterone and Adiponectin Q receptor family
02

Mechanism of action

Activation of AMP-activated protein kinase (AMPK) Activation of peroxisome proliferator-activated receptor alpha (PPAR-α) Increased fatty acid oxidation Inhibition of gluconeogenesis

03

Biological functions

Regulation of glucose and lipid metabolismActivation of AMPK pathwayActivation of PPAR-α pathwayAnti-inflammatory responseRegulation of insulin sensitivity
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Disease associations

Type 2 diabetes mellitusObesityCardiovascular diseaseInflammation and metabolic syndrome
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Safety considerations

No major safety concerns specifically documented for modulation of AdipoR1/R2, but downstream effects (e.g., excessive activation of AMPK or PPAR-α) could theoretically impact homeostasis
06

Interacting drugs

AdipoRon (an experimental AdipoR agonist, not clinically approved)

1 more in the full profile.

07

Biomarkers

Serum adiponectin levels (used as a biomarker for metabolic health)Expression levels of AdipoR1 and AdipoR2 in tissue

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